Shandong Peninsula Engineering Research Center of Comprehensive Brine Utilization, Weifang University of Science and Technology, Shouguang 262700, P. R. China.
School of Pharmacy, Weifang Medical University, Weifang 261053, P. R. China.
Org Lett. 2022 Oct 21;24(41):7492-7496. doi: 10.1021/acs.orglett.2c02589. Epub 2022 Oct 10.
Herein, we report a convenient solvent-controlled regioselective esterification to access two types of carboxylate esters without any additive or non-green activation strategy. In this transformation, 2-methyleneaziridines served as an ester reagent, providing two alternative electrophilic carbon centers. Notably, this protocol is suitable for some structure-complicated clinical molecules with a carboxylic acid group, presenting remarkable application potential.
在此，我们报告了一种方便的溶剂控制区域选择性酯化方法，无需任何添加剂或非绿色活化策略即可获得两种类型的羧酸酯。在这种转化中，2-亚甲基氮丙啶作为酯试剂，提供了两个替代的亲电碳中心。值得注意的是，该方案适用于具有羧酸基团的一些结构复杂的临床分子，具有显著的应用潜力。
